ERK2
ERK2 (MAPK1) is a core effector kinase of the Ras/Raf/MEK/ERK signaling cascade and functions as an integration point for extracellular signals that regulate cell proliferation, differentiation, survival, transcriptional programs, and development[1][2]. Mechanistically, ERK2 is activated through MEK-dependent phosphorylation and subsequently phosphorylates numerous substrates across cellular compartments, linking growth factor stimulation to broad biological responses[3]. Because ERK signaling controls fundamental cellular processes, dysregulation of the pathway is associated with multiple pathological conditions, particularly tumorigenesis, and aberrant ERK pathway activity is observed in a substantial proportion of human cancers[4]. In experimental systems, genetic disruption studies demonstrate that ERK2 is essential for normal mammalian development, as loss of ERK2 causes embryonic lethality, highlighting the critical requirement for adequate ERK signaling output[3]. Compared with the closely related isoform ERK1 (MAPK3), ERK2 shares highly conserved activation mechanisms, substrate recognition properties, and signaling functions, and many studies support the view that biological outcomes are largely determined by total ERK activity rather than strict isoform-specific functions[3]. For experimental applications, ERK pathway inhibitors targeting RAF, MEK, or ERK have been extensively developed and are widely used to investigate ERK-dependent signaling networks, disease mechanisms, therapeutic resistance, and pathway regulation in cancer models[4][5].
References:
- [1]. Mitogen Activated Protein Kinase 1. Sciencedirect topic.
- [2]. Wikipedia.
- [3]. Buscà R, et al. ERK1 and ERK2 Map Kinases: Specific Roles or Functional Redundancy? Front Cell Dev Biol. 2016 Jun 8;4:53. [Content Brief]
- [4]. Timofeev O, et al. ERK pathway agonism for cancer therapy: evidence, insights, and a target discovery framework. NPJ Precis Oncol. 2024 Mar 14;8(1):70. [Content Brief]
- [5]. Sah VK, et al. Advances in ERK1/2 inhibition: a medicinal chemistry perspective on structure and regulation. J Enzyme Inhib Med Chem. 2025 Dec;40(1):2555510. [Content Brief]
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ERK2 Related Products (228)
Related Products (228)
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Antibodies (1)
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Yoda 1
0 ImagesYoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
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PD98059
0 ImagesPD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
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Erlotinib
0 ImagesSynonyms: CP-358774; NSC 718781; OSI-774Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.
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Leupeptin hemisulfate
0 ImagesLeupeptin hemisulfate is a broad-spectrum protease inhibitor. Leupeptin hemisulfate inhibits serine, cysteine and threonine proteases, and regulates autophagy. Leupeptin hemisulfate reduces the expression levels of LC3B, iNOS, Cox-2, Beclin-1 and the level of endopeptidases; increases the levels of p62, Arg 1, Msr 1 and Mrc−1; and blocks the upregulation of p-PTEN, p-NF-κB, p-PI3K, p-Akt, p-p38 and ERK1/2. Leupeptin hemisulfate inhibits NO, ROS, proinflammatory cytokines, the IFN-γ/IL-10 ratio, phagolysosome fusion, mammalian lysosomal hydrolase activity and SARS-CoV-2 replication; and reverses impaired autophagic flux. Leupeptin hemisulfate is applicable to research related to chronic inflammatory diseases, edema, skin tumorigenesis, COVID-19 and respiratory infections.
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Mianserin hydrochloride
0 ImagesSynonyms: Org GB 94Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy.
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Mianserin
0 ImagesSynonyms: MianserineMianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
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Zoniporide hydrochloride hydrate
0 ImagesSynonyms: CP-597396 hydrochloride hydrateZoniporide hydrochloride hydrate (CP-597396 hydrochloride hydrate) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride hydrate reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride hydrate is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.
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β-Glycerophosphate disodium salt pentahydrate
0 Imagesβ-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells.
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Ulixertinib
0 ImagesSynonyms: BVD-523; VRT752271Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
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Honokiol
0 ImagesSynonyms: NSC 293100Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
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β-Glycerophosphate disodium salt hydrate
0 Imagesβ-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells.
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Desipramine hydrochloride
0 ImagesDesipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
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Piperlongumine
0 ImagesSynonyms: PiplartinePiperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.
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Temuterkib
0 ImagesSynonyms: LY3214996Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
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Gamma-Linolenic acid
0 ImagesGamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases.
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Fucoxanthin
0 ImagesFucoxanthin (all-trans-Fucoxanthin) is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
